Skip to the beginning of the images gallery

PF-5274857 - 10mM in DMSO, high purity , CAS No.1373615-35-0(DMSO)

COA

Grade & Purity:

10mM in DMSO

Cas Number: 1373615-35-0(DMSO)
Molecular Weight: 436.96

In stock

Item Number

P407918

Grouped product items
SKU	Size	Availability	Price	Qty
P407918-1ml	1ml	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$1,260.90

Smoothened Selective Inhibitors | Agonists | Antagonists

View related series

Compound libraries (12325)

Basic Description

Synonyms	1-(4-(5-chloro-4-(3,5-dimethylpyridin-2-yl)pyridin-2-yl)piperazin-1-yl)-3-(methylsulfonyl)propan-1-one
Specifications & Purity	10mM in DMSO
Biochemical and Physiological Mechanisms	PF-5274857 is a potent and selective Smoothened (Smo) antagonist, inhibits Hedgehog (Hh) signaling with IC50 and Ki of 5.8 nM and 4.6 nM, respectively, and can penetrate the blood–brain barrier.
Storage Temp	Store at -80°C
Shipped In	Ice chest + Ice pads This product requires cold chain shipping. Ground and other economy services are not available.
Product Description	Information PF-5274857 is a potent and selectiveSmoothened (Smo)antagonist, inhibitsHedgehog(Hh) signaling withIC50andKiof 5.8 nM and 4.6 nM, respectively, and can penetrate the blood–brain barrier. In vitro PF-5274857 completely inhibits Shh-induced Hh pathway activity with IC50 of 2.7 nM measured by the transcriptional activity of Smo downstream gene Gli1 in MEF cells. The μ-opioid receptor is weakly inhibited by PF-5274857 with a dissociation constant of 36 μM subsequently determined in a functional assay. In vivo PF-5274857 shows significant dose-dependent tumor growth inhibition (TGI) and induces tumor regression at high doses(>10 mg/kg)., PF-5274857 downregulates Gli1, Gli2, Ptch1, and Ptch2 gene expression levels to various degrees with maximal effects being achieved between 6 and 12 hours post-dose (Gli1 is the most sensitive gene), whereas PF-5274857 has little effect on Smo levels. In skin tissue, downregulation of Gli1 and Gli2 is also observed with a similar time course by PF-5274857. The model-derived drug concentration for half maximal inhibition of the tumor Gli1 mRNA production rate (IC50) by PF-5274857 is determined to be 8.9 nM in the Ptch^+/−p53^+/− medulloblastoma allograft mice, which mathematically corresponds to tumor regression of 119% TGI after 6 days of plasma exposure at this concentration. In the Ptch^+/−p53^−/− medulloblastoma allograft mice, the IC50 value is estimated to be 3.5 nM, consistent with the Ptch^+/−p53^+/− results. PF-5274857 is also able to cross the blood–brain barrier in rats within 4 hours post-dose. Cell Data cell lines：SW48, Colo 201, SW480, WiDr, Colo205, RKO E6, RKO, LoVo, HCT-116, SW620, HT29, W1417, DLD-1, HCT-8, Colo 320HSR, Hep-3B, OVCAR-3, MEC-1 cells Concentrations：50 pM- 3 μM Incubation Time：48 hours Powder Purity:≥97%

Associated Targets(Human)

SMO Tclin Smoothened homolog (1 Activities)

Discover Target: SMO

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

Smiles	CC1=CC(=C(N=C1)C2=CC(=NC=C2Cl)N3CCN(CC3)C(=O)CC[S](C)(=O)=O)C
Molecular Weight	436.96

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):

Analytical Chart:

Chemical and Physical Properties

Solubility	Solubility (25°C) In vitro DMSO: 57 mg/mL (197.71 mM); Ethanol: 15 mg/mL (52.02 mM); Water: Insoluble;

Solution Calculators

Molarity Calculator

Determine the necessary mass, volume, or concentration for preparing a solution.

Mass

Concentration

Volume

M. Wt*

g/mol

*When preparing stock solutions, always use the batch-specific molecular weight of the product found on the vial label and the Certificate of Analysis (available online).

Dilution Calculator

Determine the dilution needed to prepare a stock solution.

Concentration 1 (C1)

Volume 1 (V1)

Concentration 2 (C2)

Volume 2 (V2)

Reconstitution Calculator

The reconstitution calculator enables you to quickly determine the volume of a reagent needed to reconstitute your vial. Just enter the mass of the reagent and the target concentration, and the calculator will do the rest.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration